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A-1165442

Name: A-1165442
Brand: TargetMol
SKU: T14067
Rating: 4.5 (1 reviews)

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Catalog No. T14067Cas No. 1221443-94-2

A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.

A-1165442

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Catalog No. T14067Cas No. 1221443-94-2

A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$364	8-10 weeks	8-10 weeks
25 mg	$1,490	8-10 weeks	8-10 weeks
50 mg	$1,940	8-10 weeks	8-10 weeks
100 mg	$2,780	8-10 weeks	8-10 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Product Introduction

Bioactivity

Description	A-1165442 is a competitive TRPV1 antagonist. For human TRPV, the IC50 values is 9 nM.
Targets&IC50	TRPV1 (human):9 nM
In vitro	A-1165442 is a potent, competitive antagonist of recombinant human TRPV1, evidenced by its IC50 value of 9 nM when activated by capsaicin and achieves a 62% block at 30 μM in acid-evoked responses, indicating incomplete blockade. It demonstrates exceptional selectivity, exceeding 100-fold over related TRP family members (TRPA1, TRPM8, TRPV2, TRPV3) and shows minimal cross-reactivity with other receptors and channels prevalent in peripheral sensory neurons, such as P2X2/3, Cav2.2, Nav channels, and KCNQ2/3. Furthermore, A-1165442 maintains limited cross-reactivity across a broad panel of 74 cell-surface receptors, ion channels, and enzymes at 10 μM, as assessed in a comprehensive screen (CEREP)[1].
In vivo	A-1165442 demonstrates exceptional pharmacological selectivity, a favorable pharmacokinetic profile, and robust efficacy in mitigating osteoarthritis pain in rodents. Its oral administration effectively inhibits capsaicin-induced nocifensive behaviors in rats, achieving an ED50 of 9.5 μmol/kg, which corresponds to a plasma concentration of 420 ng/mL (970 nM). Furthermore, a single dose markedly enhances grip strength, with an ED50 of 35 μmol/kg observed one hour after administration. Notably, its analgesic potency increases with repeated doses. Importantly, administration of A-1165442 does not significantly alter core body temperature in conscious rats, maintaining this temperature-neutral effect in conscious dogs[1].

Chemical Properties

Molecular Weight	431.86
Formula	C₂₂H₂₀ClF₂N₃O₂
Cas No.	1221443-94-2
Smiles	Cc1cc2c(NC(=O)N[C@@H]3CC(CF)(CF)Oc4cc(Cl)ccc34)cccc2cn1
Relative Density.	1.38 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (231.56 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.64 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3156 mL	11.5778 mL	23.1557 mL	115.7783 mL
5 mM	0.4631 mL	2.3156 mL	4.6311 mL	23.1557 mL
10 mM	0.2316 mL	1.1578 mL	2.3156 mL	11.5778 mL
20 mM	0.1158 mL	0.5789 mL	1.1578 mL	5.7889 mL
50 mM	0.0463 mL	0.2316 mL	0.4631 mL	2.3156 mL
100 mM	0.0232 mL	0.1158 mL	0.2316 mL	1.1578 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc